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Assay Detail

CHEMBL617460

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity towards 5-hydroxytryptamine 2A receptor binding site using [3H]ketanserin.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
Perregaard J, Moltzen EK, Meier E, Sánchez C.
J Med Chem (1995) 38 : 1998 -2008
PubMed 7783131 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.72 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279586 1 7.85
CHEMBL59335 1 7.60
CHEMBL64344 1 7.57
CHEMBL60267 1 7.47
CHEMBL54 HALOPERIDOL 4.0 1 7.26
CHEMBL42228 1 7.18
CHEMBL61747 1 7.08
CHEMBL59940 1 6.82
CHEMBL416506 1 6.60
CHEMBL61539 1 6.57
CHEMBL59464 1 6.44
CHEMBL60859 BMY-14802 1 6.08
CHEMBL61479 SIRAMESINE 2.0 1 5.70
CHEMBL62994 1 5.43
CHEMBL303336 1 5.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279586 IC50 = 14.0 nM 7.85
CHEMBL59335 IC50 = 25.0 nM 7.60
CHEMBL64344 IC50 = 27.0 nM 7.57
CHEMBL60267 IC50 = 34.0 nM 7.47
CHEMBL54 HALOPERIDOL IC50 = 55.0 nM 7.26
CHEMBL42228 IC50 = 66.0 nM 7.18
CHEMBL61747 IC50 = 83.0 nM 7.08
CHEMBL59940 IC50 = 150.0 nM 6.82
CHEMBL416506 IC50 = 250.0 nM 6.60
CHEMBL61539 IC50 = 270.0 nM 6.57
CHEMBL59464 IC50 = 360.0 nM 6.44
CHEMBL60859 BMY-14802 IC50 = 830.0 nM 6.08
CHEMBL61479 SIRAMESINE IC50 = 2000.0 nM 5.70
CHEMBL62994 IC50 = 3700.0 nM 5.43
CHEMBL303336 IC50 = 7100.0 nM 5.15